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Ccr5 antagonists as prophylactics for preventing HIV infection and methods of inhibiting transmission of same

a technology of ccr5 and anti-histamine, which is applied in the field of topical formulations or preparations, can solve the problems of inability to prove clinically effective anti-histamine microbicides, limited development of some of these early microbicides, irritation or disruption of mucosal tissues,

Inactive Publication Date: 2011-03-10
MERCK SHARP & DOHME CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patent describes a topical formulation that contains a small molecule CCR5 receptor antagonist for the treatment of vaginal, rectal or buccal administration. The formulation can be in the form of a cream, gel, ointment, foam, tablet or film. The CCR5 receptor antagonist can also be present in a vaginal ring device, an IUD or a sponge. The invention provides a new way to treat HIV and other sexual transmitted infections.

Problems solved by technology

Although the idea has been around for many years, no microbicide has yet proved clinically effective against HIV.”).
However the development of some of these early microbicides may be limited by factors such as limited absorption, irritation or disruption of mucosal tissues, agent stability or cost.

Method used

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  • Ccr5 antagonists as prophylactics for preventing HIV infection and methods of inhibiting transmission of same
  • Ccr5 antagonists as prophylactics for preventing HIV infection and methods of inhibiting transmission of same
  • Ccr5 antagonists as prophylactics for preventing HIV infection and methods of inhibiting transmission of same

Examples

Experimental program
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formulation examples

Example 1

[0344]A vaginal cream formulation is prepared by mixing the components listed in Table 1 below. For each application, 1-4 grams of the cream are vaginally administered with a suitable applicator such as a syringe.

TABLE 1ComponentWeight PercentCompound Va10-40Cetyl esters wax 1-15Cetyl alcohol2-5White wax 5-20Glyceryl monostearate10-30Propylene glycol10-15monostearateMethyl stearate 5-90Benzyl alcohol 3-10Sodium lauryl sulfate0.5-2.5Glycerin 5-30Mineral oil0.1-95 

example 2

[0345]A vaginal cream formulation is prepared by mixing the components listed in Table 2 below. For each application, 1-4 grams of the cream are vaginally administered with a suitable applicator such as a syringe.

TABLE 2ComponentWeight PercentCompound IIIa10-40edetate disodium0.01-0.10glyceryl0.5-10 monoisostearatemethyl paraben0.18-0.20mineral oil0.1-95 polyglyceryl-3-oleate  2-3.5propylene glycol 5-15propyl paraben0.02-0.10colloidal silicon dioxide1-5sorbitol solution 2-18purified water10-20microcrystalline wax 2-20

example 3

[0346]A vaginal gel formulation is prepared by mixing the components listed in Table 3 below. For each application, 4 grams of the gel are vaginally administered with a suitable applicator such as a syringe.

TABLE 3ComponentWeight PercentCCR5 antagonist of any10-40Formulas I-XICarbomer 934P0.1-0.5Edetate disodium0.01-0.10Methyl paraben0.18-0.20Propyl paraben0.02-0.10Propylene glycol 5-15Sodium hydroxide0.01-0.05

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Abstract

Topical cream, ointment, lotion, gel, foam formulations and slow release formulations or devices are provided including certain CCR5 antagonists as prophylactics for the prevention, retardation or inhibition of transmission of Human Immunodeficiency Virus (HIV) infection from one human to another.

Description

FIELD OF THE INVENTION[0001]The present invention relates to topical formulations or preparations comprising certain CCR5 antagonists as prophylactics for Human Immunodeficiency Virus (“HIV”) infection, such as vaginal or rectal topical preparations for use in preventing HIV infection or inhibiting transmission of HIV.BACKGROUND OF THE INVENTION[0002]Citation of any reference in this section or any other section in this application shall not be deemed an admission that such reference is available as prior art to this application.[0003]The lack of proper medicaments to prevent and / or stop the spread of HIV among sexual partners has been well documented. See, for example, (1) J. Cohen, Science, (Oct. 15, 2004) 306, page 387 (“Microbicides have long had a stepchild status in the AIDS research community. Industry has had little interest in developing a topical gel or cream that can stop HIV at the vagina or rectum, and the products that have moved furthest in human studies are soaps and...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61F6/06C07D401/14A61K31/4545C07D403/04A61K31/506A61P31/18
CPCA61K9/0014A61K9/0031A61K9/0034A61K31/15A61K31/165A61K31/506A61K31/44A61K31/4425A61K31/4545A61K31/497A61K31/18A61P31/18A61P43/00
Inventor STRIZKI, JULIE M.
Owner MERCK SHARP & DOHME CORP
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